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Looking Under the Lamppost: The Search for New Cancer Targets in the Human Kinome

Sueca-Comes, Mireia; Rusu, Elena Cristina; Grabowska, Anna M.; Bates, David O.

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Mireia Sueca-Comes

Elena Cristina Rusu

Professor of Cancer Microenvironment

Professor of Oncology



The number of cancer drugs is increasing as new chemical entities are developed to target molecules, often protein kinases, driving cancer progression. In 2009, Fedorov et al. identified that of the protein kinases in the human kinome, most of the focus has been on a small subset. They highlighted that many poorly investigated protein kinases were cancer drivers, but there was no relationship between publications and involvement in cancer development or progression. Since 2009, there has been a doubling in the number of publications, patents, and drugs targeting the kinome. To determine whether this was an expansion in knowledge of well-studied targets-searching in the light under the lamppost-or an explosion of investigations into previously poorly investigated targets, we searched the literature for publications on each kinase, updating Federov et al.'s assessment of the druggable kinome. The proportion of papers focusing on the 50 most-studied kinases had not changed, and the makeup of those 50 had barely changed. The majority of new drugs (80%) were against the same group of 50 kinases identified as targets 10 years ago, and the proportion of studies investigating previously poorly investigated kinases (<1%) was unchanged. With three exceptions [p38 mitogenactivated protein kinase (p38a), AMP-activated protein kinase catalytic α-subunit 1,2, and B-Raf proto-oncogene (BRAF) serine/threonine kinase], >95% of publications addressing kinases still focused on a relatively small proportion (<50%) of the human kinome independently of their involvement as cancer drivers. There is, therefore, still extensive scope for discovery of therapeutics targeting different protein kinases in cancer and still a bias toward well-characterized targets over the innovative searchlight into the unknown. SIGNIFICANCE STATEMENT: This study presents evidence that drug discovery efforts in cancer are still to some extent focused on a narrow group of well-studied kinases 10 years after the identification of multiple novel cancer targets in the human kinome. This suggests that there is still room for researchers in academia, industry, and the not-for-profit sector to develop new and diverse therapies targeting kinases for cancer.


Sueca-Comes, M., Rusu, E. C., Grabowska, A. M., & Bates, D. O. (2022). Looking Under the Lamppost: The Search for New Cancer Targets in the Human Kinome. Pharmacological Reviews, 74(4), 1136-1145.

Journal Article Type Article
Acceptance Date Feb 15, 2022
Online Publication Date Sep 30, 2022
Publication Date Oct 1, 2022
Deposit Date Feb 24, 2022
Publicly Available Date Sep 30, 2022
Journal Pharmacological reviews
Print ISSN 0031-6997
Electronic ISSN 1521-0081
Publisher American Society for Pharmacology & Experimental Therapeutics (ASPET)
Peer Reviewed Peer Reviewed
Volume 74
Issue 4
Pages 1136-1145
Keywords Pharmacology; Molecular Medicine
Public URL
Publisher URL


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